111 results about "Fluoxetine" patented technology

The subject invention provides methods for treating symptoms and / or conditions associated with idiopathic hyperhidrosis by using compounds that decrease the activity of serotonin 5-HT2C receptors. Compounds that can ameliorate symptoms of idiopathic hyperhidrosis and associated conditions include 5-HT2C receptor antagonists (i.e., ketanserin, ritanserin, mianserin, mesulergine, cyproheptadine, fluoxetine, mirtazapine, olanzapine, and ziprasidone) as well as 5-HT2C receptor modulators (i.e., inverse agonists, partial agonists, and allosteric modulators).

One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., insomnia and / or depression. The first component of the pharmaceutical composition is a GABA receptor modulating compound. The second component of the pharmaceutical composition is a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a 5-HT2A modulator, or dopamine reuptake inhibitor. In certain embodiments, the pharmaceutical composition comprises eszopiclone. In a preferred embodiment, the pharmaceutical composition comprises eszopiclone and fluoxetine. The present invention also relates to a method of treating a sleep abnormality, treating insomnia, treating depression, augmenting antidepressant therapy, eliciting a dose-sparing effect, reducing depression relapse, improving the efficacy of antidepressant therapy or improving the tolerability of antidepressant therapy, comprising co-administering to a patient in need thereof a GABA-receptor-modulating compound; and a SRI, NRI, 5-HT2A modulator or DRI.

Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and / or preventing pulmonary arterial hypertension and / or stable angina. More particularly, aspects of the present invention are related to therapeutic combinations comprising a Rho-kinase inhibitor, such as fasudil, and one or more additional compounds selected from the group consisting of prostacyclins, such as iloprost, endothelin receptor antagonists, PDE inhibitors, calcium channel blockers, 5-HT2A antagonists, such as sarpogrelate, selective serotonin reuptake inhibitors, such as fluoxetine, statins, and vascular remodeling modulators, such as Gleevec.

The present invention provides compositions and methods for extending the release times and lowering the toxicity of pharmacologically active compounds. The compounds comprise a salt of the pharmacologically active compound with a lipophilic counterion and a pharmaceutically acceptable water soluble solvent combined together to form an injectable composition. The lipophilic counterion may be a saturated or unsaturated C8-C22 fatty acid, and preferably may be a saturated or unsaturated C10-C18 fatty acid. When injected into a mammal, at least a portion of the composition precipitates and releases the active compound over time. Thus, the composition forms a slowly releasing drug depot of the active compound in the mammal. Therefore, the present invention enables one to provide a controlled dose administration of the active compound for a periods of up to 15 days or even longer. Many compounds can be administered according to the present invention including, but not limited to, tilmicosin, oxytetracycline, metoprolol, fluoxetine, roxithromycin, and turbinafine.

Composition of matter for application to a body surface or membrane to administer fluoxetine by permeation through the body surface or membrane, the composition comprising fluoxetine to be administered, at a therapeutically effective rate, alone or in combination with a permeation enhancer or mixture. A preferred embodiment is directed to the transdermal administration of fluoxetine at reduced skin irritation levels wherein fluoxetine, preferably provided as fluoxetine acetate, is coadministered with a corticosteroid such as hydrocortisone. Also disclosed are drug delivery devices containing the fluoxetine or fluoxetine and enhancer composition and methods for the transdermal administration of the fluoxetine and fluoxetine / enhancer composition.

One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., insomnia and / or depression. The first component of the pharmaceutical composition is a GABA receptor modulating compound. The second component of the pharmaceutical composition is a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a 5-HT2A modulator, or dopamine reuptake inhibitor. In certain embodiments, the pharmaceutical composition comprises eszopiclone. In a preferred embodiment, the pharmaceutical composition comprises eszopiclone and fluoxetine. The present invention also relates to a method of treating a sleep abnormality, treating insomnia, treating depression, augmenting antidepressant therapy, eliciting a dose-sparing effect, reducing depression relapse, improving the efficacy of antidepressant therapy or improving the tolerability of antidepressant therapy, comprising co-administering to a patient in need thereof a GABA-receptor-modulating compound; and a SRI, NRI, 5-HT2A modulator or DRI.

The present invention provides compositions and methods for extending the release times and lowering the toxicity of pharmacologically active compounds. The compounds comprise a salt of the pharmacologically active compound with a lipophilic counterion and a pharmaceutically acceptable water soluble solvent combined together to form an injectable composition. The lipophilic counterion may be a saturated or unsaturated C8-C22 fatty acid, and preferably may be a saturated or unsaturated C10-C18 fatty acid. The compounds precipitate in aqueous environments. When injected into a mammal, at least a portion of the composition precipitates and releases the active compound over time. Thus, the composition forms a slowly releasing drug depot of the active compound in the mammal. Therefore, the present invention enables one to provide a controlled dose administration of the active compound for a period of up to 15 days or even longer. Many compounds can be administered according to the present invention including, but not limited to, tilmicosin, oxytetracycline, metoprolol, fluoxetine, roxithromycin, and turbinafine.

The invention relates to application of tetrahydrocurcumin in preparing an antidepressant and a method for preparing a solid dispersion of the tetrahydrocurcumin. The invention aims to provide the application of the tetrahydrocurcumin to prepare the antidepressant. The tetrahydrocurcumin and a surfactant are mixed in certain proportion to obtain the solid dispersion of the tetrahydrocurcumin. The method for preparing the solid dispersion of the tetrahydrocurcumin comprises the following steps that: according to the weight ratio of 1:3-1:30, the tetrahydrocurcumin and the surfactant are heated until completely melted, frozen in a low-temperature environment, and taken out, dried and crushed to obtain the solid dispersion of the tetrahydrocurcumin. The tetrahydrocurcumin and the solid dispersion of the tetrahydrocurcumin are used for preparing drugs, health care products, foods or food additives of relieving mental depression. The tetrahydrocurcumin has the function of relieving mental depression, and the function of the tetrahydrocurcumin is possibly related with the influence on a monoamine neurotransmitter system; moreover, compared with fluoxetine, the tetrahydrocurcumin has the advantages of low toxicity and good curing effect.

Composition of matter for application to a body surface or membrane to administer fluoxetine by permeation through the body surface or membrane, the composition comprising fluoxetine to be administered, at a therapeutically effective rate, alone or in combination with a permeation enhancer or mixture. A preferred embodiment is directed to the transdermal administration of fluoxetine at reduced skin irritation levels wherein fluoxetine, preferably provided as fluoxetine acetate, is coadministered with a corticosteroid such as hydrocortisone. Also disclosed are drug delivery devices containing the fluoxetine or fluoxetine and enhancer composition and methods for the transdermal administration of the fluoxetine and fluoxetine / enhancer composition.

The invention relates to an oral traditional Chinese medicine preparation for treating melancholia and anxiety neurosis, which is prepared by adopting the following raw materials of traditional Chinese medicines in parts by weight: 15+ / -3 of roasted astragalus root, 10+ / -2 of American ginseng, 10+ / -2 of white atractylodes rhizome, 10+ / -2 of tall gastrodia tuber, 10+ / -2 of medlar, 10+ / -2 of prepared rehmannia root, 10+ / -2 of white peony root, 10+ / -2 of radix salviae miltiorrhizae, 10+ / -2 of angelica, 10+ / -2 of rhizoma ligustici wallichii, 10+ / -2 of herba epimedii, 15+ / -3 of spine date seed, 10+ / -2 of tuckahoe, 10+ / -2 of rhizoma anemarrhenae, 10+ / -2 of rhizoma cyperi, 10+ / -2 of radix bupleuri, 10+ / -2 of TurmericRoot-tuber and 6+ / -1.2 of roasted licorice. The observation of clinical curative effect proves that the total effective rate of the invention for treating the anxiety neurosis is 92.2%; the total effective rate of the invention for treating the melancholia is 91.0%. The curative effect of the oral traditional Chinese medicine preparation is similar to the curative effect of the western medicines of buspirone for treating the anxiety neurosis and fluoxetine for treating the melancholia. Moreover, the traditional Chinese medicine preparation has no obvious toxic or side effect and can be taken for a long time. The preparation has small dose, easy release of the effective components of the medicine, quick absorption, full exertion of the medicine effect, convenient carrying and easy taking and is beneficial to large-scale production.

The invention discloses a drug for treating depression. The drug contains an effective amount of 4-{4-(4-fluorophenyl)-1-[1-(isoxazole-3-ylmethyl)piperidine-4-yl]-1H-imidazole-5-yl}pyrimidine-2-amine and an effective amount of fluoxetine, and the mass ratio of 4-{4-(4-fluorophenyl)-1-[1-(isoxazole-3-ylmethyl)piperidine-4-yl]-1H-imidazole-5-yl}pyrimidine-2-amine to fluoxetine is 3:1 to 6:1. Through combined use of specific drugs, side effects during treatment of depression are greatly reduced, pain of patients is reduced, and recovery of the patients is availed.

The invention relates to a fluoxetine capsule and a preparation method thereof. The capsule is composed of certain proportion of active component, microcrystal fiber and pregelatinized starch. In the environment that relative humidity is not more than 75%, the components are mixed, smashed and sieved, and the mixture is packaged into empty capsules after uniformity degree is detected to be qualified, thus obtaining the fluoxetine capsule. The capsule can be used for treating mental disease. The fluoxetine capsule provided by the invention has the characteristics of simple preparation process, low cost and easy industrialization production.

The invention relates to a composite which is composed of (2Z, 8Z, 10E)-2,8,10-pentadecane triene-4,6-diyne-1-alcohol and (2Z, 8E, 10E)-2,8,10-pentadecane triene-4,6-diyne-1-alcohol according to the proportion of 1:(1-4) or is composed of (2Z, 8Z, 10E)-2,8,10-heptadecane triene-4,6-diyne-1-alcohol and (2Z, 8E, 10E)-2,8,10-heptadecane triene-4,6-diyne-1-alcohol according to the proportion of 1:(1-4). The composite disclosed by the invention is obtained by being extracted and separated from traditional Chinese medicine radix bupleuri. The result of an in-vitro monoamine neurotransmitter reuptake inhibition experiment shows that the composite disclosed by the invention has triple inhibition effects on the reuptake of 5-HT (5-Hydroxytryptamine), NA (noradrenalin) and DA (Dopamine), is higher than the effective part of ease powder petroleum ether and the part of radix bupleuri petroleum ether in inhibition ratio and is higher than positive control drugs, namely fluoxetine, norpramin and 6-hydroxydopamine, in inhibiting effect. According to the invention, two composites can be applied to prepare a drug used for preventing and curing depression.

The invention belongs to the technical field of a medicinal preparation, and relates to a fluoxetine ointment for treating leucoderma. The ointment is prepared by combination of Chinese traditional and western medicines. A preparation method of the ointment comprises the following steps: extracting the traditional Chinese medicinal material active ingredients by an ultrasonic method for standby, dissolving fluoxetine in propylene glycol for standby; adding a certain amount of water-phase component and an emulsifier in a certain amount of an oil-phase component for being stirred to obtain an emulsifiable paste matrix; and finally adding the medicine and an antiseptic into the matrix to obtain the finished product. The preparation method is simple, and the treatment effect is obvious.

Provided is an efficient method for the preparation of 3-aryloxy-3-arylpropylamines, their optical stereoisomers, and pharmaceutically acceptable salts thereof. The process allows for the isolation of 3-aryloxy-3-arylpropylamines in high yield and purity. The present invention further relates to a process for producing fluoxetine, tomoxetine, norfluoxetine, duloxetine, nisoxetine, and their optically enriched (R)- and (S)-enantiomers.

Method for the treatment of psychiatric disorders, comprising administering to a subject in need thereof an amount of fatty acids and a suboptimal dose of at least one antidepressant. Wherein the fatty acid may be omega-3 (ω3), for example the docohexaenoic acid (DHA) and the eicosapentaenoic acid (EPA). The omega-3 fatty acid may be administered orally, in amounts that may be variable, for example in amounts between 0.15 and 1.00 g / kg / day. The antidepressant may be any antidepressant, preferably the antidepressant is fluoxetine or mirtazapine in sub-optimal doses.

The invention provides an antidepressant traditional Chinese medicine composition, which is prepared from the following components in parts by weight: 15-50 parts of gypsum, 3-10 parts of rhizoma anemarrhenae, 10-30 parts of uncaria rhynchophylla, 3-10 parts of radix ophiopogonis, 5-15 parts of rehmanniae praeparatum, 5-15 parts of Inula japonica, 3-15 parts of officinal magnolia bark, 3-15 parts of medicinal cyathula root, 3-10 parts of raw hematite,10-30 parts of rhizoma phragmitis, 3-10 parts of immature bitter orange and 3-12 parts of semen raphani. The antidepressant traditional Chinese medicine composition in the invention has the following beneficial effects: (1) the composition can cure depression effectively; (2) as for curative effect, the composition is similar to or stronger than fluoxetine hydrochloride, and the composition has the functions of invigorating food stagnation and relaxing bowel; (3) as for price, the cost of the composition is lower than that of fluoxetine hydrochloride; and (4) in long-term clinic observation, side effects such as excitement, anxiety, thirsty, hydrosis, headache, drowsiness in day, insomnia at night, astriction and sexual dysfunction, damaged liver kidney function and the like do not occur.

The invention relates to a method for preparing antidepressant fluoxetine, and belongs to the method for preparing a medicinal compound. The technical scheme in the invention comprises the following three steps of aminolysis, catalytic hydrogenation and aromatic etherification reaction, wherein the three steps are performed in one pot without separation. In the method, the conventional chemical reduction method is replaced by the catalytic dehydration process, and the used reducing agent is hydrogen gas, so that the environmental pollution is reduced; the methylamine is gaseous methylamine, so that the reaction conversion rate is improved, and other substances, such as water and the like, are prevented from being introduced into a reaction system; and p-chlorobenzotrifluoride is added dropwise in the etherification reaction, so that the reaction speed can be conveniently controlled, the yield of a target product is improved, and the possibility of catalyst poisoning is reduced.

The invention discloses benzothiophene alkanol piperazine derivatives and their use as antidepressants. The invention discloses the said benzothiophene alkanol piperazine derivative having triple inhibition effect on the reuptake of 5-HT, NA and DA. Compared with clinical used antidepressants so far having single target, e.g. desipramine and fluoxetine, and clinical used antidepressants so far having double targets, e.g venlafaxine and duloxetine, the said benzothiophene alkanol piperazine derivatives of the present invention may have a broader indication range and less toxic and side effects to nervous system. The benzothiophene alkanol piperazine derivatives are the compounds with the following formula or their pharmaceutically acceptable salts, wherein Ar1, R1-R4, X, Y, m and n have the same definition as defined in claim 1.

The invention relates to the technical field of medicines, and in particular to an application of andrographolide in preparing medicines for treating depression. Based upon researches with the assistance of various depression animal models and test methods, the andrographolide, through intraperitoneal injection, can obviously reverse various depression-like behaviors caused by the depression models, with efficacy intensity not weaker than that of a classical clinical anti-depression medicine, namely fluoxetine; therefore, as a completely new pharmacological effect, the andrographolide can be used for effectively relieving and treating the depression.

The invention discloses a method for producing (S)-3-chlorobenzene phenylpropanol through carbonyl reductase catalysis. The method is characterized by comprises the following steps: utilizing existingcarbonyl reductase as a catalyst; performing catalytic production on a substrate 3-chlorobenzene phenylpropanol to produce high-chirality ee (larger than 99) value (S)-fluoxetine intermediate (S)-3-chlorobenzene phenylpropanol; utilizing carbonyl reductase ChKRED20 as a catalyst, wherein a reaction system comprises a pH equal to 6.0 to 8.0, a 0.1M potassium phosphate buffer solution, the carbonylreductase ChKRED20, NADH (reduced coenzyme I) or NADPH (reduced coenzyme II) and the substrate. According to the method disclosed by the invention, a biological-enzyme catalytic method is utilized for preparing the high-chirality ee (larger than 99) value (S)-fluoxetine intermediate (S)-3-chlorobenzene phenylpropanol, a traditional chemical synthesizing method is replaced, and production cost andenvironmental pollution are reduced.

The invention discloses an application of aporphine alkaloid shown in a formula III in preparation of an antidepressant drug. R1 and R2 are respectively and independently selected from alkoxy and methylenedioxy, R3 and R4 are respectively and independently selected from H, OH, alkoxy and methylenedioxy, but when R3 and R4 cannot be H at the same time or R1 and R2 are both selected from methoxy, R3 cannot be OH, and R4 cannot be H. Pharmacological experiments show that the aporphine alkaloid shown in the formula III has a better anti-depression drug effect, and compared with fluoxetine, the aporphine alkaloid has a better anti-depression effect, a higher response rate and a faster effect.

The present invention provides a pharmaceutical composition comprising a selective serotonin reuptake inhibitor (SSRI) and a norepinephrine reuptake inhibitor (NRI), particularly, fluoxetine and reboxetine, for treating obesity. Surprisingly, the inventor of the present invention discovered that use of especially low doses of the active compounds, particularly, at most 6 mg / day of reboxetine and at most 20 mg / day of fluoxetine, wherein the reboxetinerfluoxetine ratio is from about 1:4 to about 1:6, induces an effective weight loss in obese patients. Advantageously, the combinations of the present invention include very low doses of the active ingredients, thereby decreasing possible drug-drug interactions and adverse drug reaction.

The invention relates to L-tryptophan asiatic acid amide (X4) and applications thereof in preparation of antidepressant medicines, and also provide a pharmaceutical composition comprising the L-tryptophan asiatic acid amide. Experiments show that: the L-tryptophan asiatic acid amide and the pharmaceutical composition thereof are safe, efficient, stable and cheap medicines for preventing and treating depression, have high activity, are superior to asiatic acid and fluoxetine, and have high development value.

The invention discloses a preparation method of flomoxef sodium. The preparation method comprises the following steps of dropwise adding a sodium bicarbonate solution into flomoxef acid while stirring at the temperature of 0-10 DEG C until the pH value of a reaction solution is up to 4.2-5.2, and after flomoxef acid is completely dissolved, extracting, decoloring and removing a decolorizing agent to obtain flomoxef sodium. By using the preparation method of flomoxef sodium, provided by the invention, flomoxef sodium can be effectively and uniformly produced in real time, the residues of sodium salt and flomoxef acid in a product are avoided, the purity of obtained flomoxef sodium is larger than or equal to 99%, and the residual quantity of 1-ethoxyl-5-thiol-1H-tetrazole is smaller than or equal to 0.2%, therefore, the standard requirement of Japanese pharmacopoeia JP16 is completely met.

Pharmaceutical formulations of fluoxetine or an acid addition salt thereof, suitable for manufacturing dispersible tablets by direct compression and comprising, in addition to the active ingredient, the appropriate excipients and coadjuvants, selected from among disintegrants, diluents, lubricants, anti-adherents, sweeteners, flavorings and, optionally, colorants. Said formulations are suitable for manufacturing dispersible tablets which disintegrate in less than three minutes in water at 19 DEG C - 21 DEG C, and are appropriate for treatment of depression.

The invention relates to an alcohol-soluble homogeneous polysaccharide and an anti-depression application thereof, in particular to a dendrobium officinale flower alcohol-soluble homogeneous polysaccharide, a preparation method thereof and an application of the dendrobium officinale flower alcohol-soluble homogeneous polysaccharide in preparation of an anti-depression drug. The alcohol-soluble homogeneous polysaccharide is obtained by purifying separated components of a natural plant aqueous extract for multiple times, and the alcohol-soluble homogeneous polysaccharide is named as ASP (Alcohol-soluble polysaccharide); and in-vivo experiments prove that the alcohol-soluble homogeneous polysaccharide has remarkable anti-depression activity, the action effect of the alcohol-soluble homogeneous polysaccharide is equivalent to that of fluoxetine serving as an anti-depression marketing drug, and the alcohol-soluble homogeneous polysaccharide can be further developed and prepared into the anti-depression drugs.

The invention relates to a drug compound for resisting against anxiety and improving sleep and an application thereof. The drug compound comprises the following active ingredients: tandospirone citrate, fluoxetine and sertraline hydrochloride. According to the invention, the tandospirone citrate, fluoxetine and sertraline hydrochloride are jointly used for treating anxiety disorder and insomnia, the defects of poor drug effect and easiness in generating drug dependence of the patient of single drug usage are overcome, the joint use of three drugs has the synergic effects of resisting against anxiety and improving sleep and the function of reducing toxicity can be achieved in the manner of reducing the clinical dosage of one or two drugs.